Abstract
A number of mono- or diaminoalkylated indeno[1,2-c]isoquinolin-5,11-diones analogs of 1 were synthesized and evaluated for their DNA binding affinities, topoisomerase inhibition properties and antiproliferative activities against human cancer cell lines (HL60). Impact of the side chain connected to the aromatic D ring and to the N6 lactam position on the biological profile will be discussed.
Copyright © 2011 Elsevier Ltd. All rights reserved.
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / toxicity
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Cell Line, Tumor
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DNA Topoisomerases, Type I / chemistry*
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DNA Topoisomerases, Type I / metabolism
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DNA Topoisomerases, Type II / chemistry*
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DNA Topoisomerases, Type II / metabolism
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Humans
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Isoquinolines / chemical synthesis
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Isoquinolines / chemistry*
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Isoquinolines / pharmacology
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Structure-Activity Relationship
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Topoisomerase I Inhibitors / chemical synthesis*
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Topoisomerase I Inhibitors / chemistry
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Topoisomerase I Inhibitors / toxicity
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Topoisomerase II Inhibitors / chemical synthesis*
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Topoisomerase II Inhibitors / chemistry
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Topoisomerase II Inhibitors / toxicity
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Transition Temperature
Substances
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Antineoplastic Agents
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Isoquinolines
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Topoisomerase I Inhibitors
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Topoisomerase II Inhibitors
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DNA Topoisomerases, Type I
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DNA Topoisomerases, Type II